Term
|
Definition
-strong agonist at kappa receptors
- partial agonist at mu receptors
- mu antagonists at high doses
- sedation//respiratory distress less than morphine
- CNS stimulation and hallucinations
- precipitate withdrawal symptoms in addicts |
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Term
|
Definition
- antagonist at ALL types of opioid receptors
- Tx opioid poisoning: reverse respiratory depression
- Must be given parenterally
- sometimes given w/ oral narcotics to prevent abuse
- Short duration: 1-2 hours
- precipitates withdrawal in addicts |
|
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Term
| Pharmacologic Actions of Morphine |
|
Definition
- analgesia
- sedation and mental clouding
- relief of anxiety
- euphoria (occasional dysphoria)
- Nausea (stimulation of CRTZ in medulla)
- respiratory depression (useful in pulm. edema however)
- Meiosis
- antitussive effect (medulla cough control center)
- release of histamine (caution with asthma; itching)
- lowering of seizure threshold
- endocrine disturbances (decreased secretions; impotence and menstrual disruptions)
- increase tone of circular SM; decrease long. SM:
- decreased peristalsis --> constipation
- urine retention
- bronchoconstriction
- increased biliary pressure (constriction of bile duct)
- inhibition of uterine contractions
- postural hypotension (histamine vasodilates)
- cutaneous vasodilation --> flushed skin, pruritis
- increased CSF pressure (CO2 buildup --> vasodilation)
- skeletal muscle rigidity
- immunosuppresion |
|
|
Term
| Drug interactions of Morphine |
|
Definition
- additive effects w/ CNS depressants
- MAO inhibitors: severe hyperpyrexemia and coma
- mix with cocaine/amphetamines "speedball"
- combo w/ other analgesics
- antihistamines can enhance analgesic effects of opioids
- tricyclic antidepressants can enhance analgesic effects of opioids |
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Term
|
Definition
- pin point pupils
- CNS depression (stupor or coma)
- decreased rate and depth of respiration |
|
|
Term
|
Definition
- given SC, IM, IV (orally = less effective)
- 10 mg dose
- half life = 2-3 hours
- liver metabolized
- 90% excreted in urine (metabolites) 10% in feces
- readily crosses placental barrier |
|
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Term
|
Definition
- orally effective
- 1/12 potency of morphine
- dosage = 30-60 mg
- use: analgesic (mild-moderate pain) and antitussive
- most patients: small % of codeine is demethylated to morphine --> effects |
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Term
|
Definition
| similar to morphine but MORE POTENT |
|
|
Term
|
Definition
- cross b/w morphine and codeine
- given orally w/ or w/o acetaminophen
- moderate-severe pain |
|
|
Term
|
Definition
- similar to codeine and oxycodone
- orally in combo with acetaminophen for mild-moderate pain
- antitussive
- one of most widely prescribed opioids |
|
|
Term
|
Definition
- synthetic drug
- given orally and parenterally
- 1/10 potency of morphine
- weaker effects on SM --> less constipation/retention
- moderate - severe pain
- used in OB: less respiratory depression in newborn
- short acting: 1-3 hours
- build up of active metabolite can cause seizures --> not acceptable for long term Tx |
|
|
Term
|
Definition
- more potent and euphoric than morphine
- 4-6 hour duration (same as morphine)
- injection, snorting, smoking |
|
|
Term
|
Definition
- less euphoric
- longer duration of action: 12-24 hours
- analgesic or Tx opioid addiction
- acute use: duration 4-6 hours; chronic 12-24 |
|
|
Term
| Levo-alpha-acetylmethadol (ORLAAM) |
|
Definition
- Tx opioid depedence
- similar to methadone but given EVERY OTHER DAY
- only dispensed through drug abuse programs |
|
|
Term
|
Definition
- much less potent than other gents
- little analgesic activity
- potential for SERIOUS cardiac toxicity at high doses
- not a good drug; withdrawn from market |
|
|
Term
|
Definition
- very potent mu agonist
- given parenterally to supplement Sx anesthesia
- transdermal prep (Duragesic) for chronic pain
- Lozenge prep for "breakthrough" pain
- fentanyl + droperidol = neuroleptic analgesia |
|
|
Term
| Sufentanil and Alfentanil |
|
Definition
- similar to fentanyl
- used IV as adjuncts for Sx anesthesia |
|
|
Term
|
Definition
- Codeine/Acetaminophen
- Codeine/Aspirin
- Hydrocodone/Acetaminophen
- Hydrocodone/Ibuprofen
- Oxycodone/Acetaminophen |
|
|
Term
|
Definition
| - similar to pentazocine (kappa agonist; partial mu agonist/antagonist at high doses) |
|
|
Term
|
Definition
- partial mu agonist (antagonist at high doses)
- analgesic effects less than morphine but abuse potential MUCH LOWER
- can reduce drug craving in heroin addicts
- given IV, sublingual, intranasal
- ***"Office based" Tx of opioid addiction! |
|
|
Term
|
Definition
- mild-moderate pain
- weak mu agonist
- inhibits re-uptake of serotonin and NE
- good analgesic w/ mild side effects
- low abuse and addiction potential |
|
|
Term
|
Definition
- very similar to naloxone
- Tx opioid poisoning
- longer duration: 2-6 hours (naloxone is 1-2) |
|
|
Term
|
Definition
- orally effective (naloxone is not)
- long acting opioid antagonist (24 hours)
- "immunizes" addicts; prevents the high
- risk of hepatotoxicity
- addict must 1st be detoxed before naltrexone given
- decrease alcohol cravings |
|
|
Term
|
Definition
- Tx/prevention opioid-induced constipation
- given parenterally
- serious constipation or post-op paralytic ileus |
|
|
Term
|
Definition
- similar to methylnaltrexone (Tx opioid induced constipation)
- better oral efficacy |
|
|
Term
|
Definition
- AED
- potentiation of GABA-A receptors
- partial seizures
- generalized tonic-clonic
-status epilepticus (IV)
- SE: sedation (adults) hyperactivity (kids); induction of CYP3A4 |
|
|
Term
|
Definition
- AED
- partial seizures
- gen. tonic/clonic
- status epilepticus: proddrug fosphenytoin
- prolong rate of Na+ channel recovery
- drug concentration increases disproportionately as dosage increases
- side effects: metabolism of CYP2C9/10/19 drugs, CYP3A4 induction, gingival hyperplasia, SJS!
- neural tube deformities in pregnancy |
|
|
Term
| AEDs which block Na+ channels |
|
Definition
V-COP:
- Valproic Acid
- Carbamazepine
- Oxycarbamazepine
- Phenytoin |
|
|
Term
| AED's that block T-type Ca2+ channels |
|
Definition
- Valproic acid
- ethosuximide |
|
|
Term
| AED's that enhance inhibitory effects of GABA |
|
Definition
- Bartbiturates: Phenobartbital and primidone
- Benzodiazepines: clonazepam, diazepam |
|
|
Term
|
Definition
- prolong rate of Na+ channel recovery
- partial seizures
- gen. tonic/clonic
- manic-depressive pts.
- induces its own metabolism
- acute side effects: stupor, coma, convulsions
- chronic side effects: drowsiness, vertigo, ataxia, blurred vision, CYP3A4 induction |
|
|
Term
|
Definition
- partial seizures
- prolong rate of Na+ recovery
- does NOT autoinduce like carpamazepine
- Side effects: dizziness, nausea, somnolence, ataxia, CYP3A4 induction |
|
|
Term
|
Definition
- monoTx for ABSENCE seizures
- inhibits Ca2+ channels
- Side effects: nausea, vomiting, anorexia, drowsiness, lethargy, euphoira, SJS, aplastic anemia |
|
|
Term
|
Definition
- MonoTx for absence, partial, myclonic, tonic/clonic "broad spectrum" AED
- IV or oral
- inhibit T-type Ca2+ channels
- prolong inactivation of Na+ channels
- increase GABA synthesis in vitro
-90% plasma protein bound therefore long half life (15 hours) but decreased when other AEDs in use
- Side effets: nausea, anorexia, sedation, ataxia, tremor
- Increased hepatic enzymes; hepatotoxicity
- inhibits CYP2C9 --> increased concentrations of phenytoin, phenobarbital; displaces phenytoin from plasma binding proteins
- TERATOGENIC!! |
|
|
Term
|
Definition
- GABA molecule bound to lipophilic hexane ring
- neuropathic pain
- partial seizures Tx (with or without generalized secondary)
- not metabolized; excrete unchanged in urine
- side effects: fatigue, ataxia |
|
|
Term
|
Definition
- "broad spectrum" AED: partial, tonic/clonic, LGS
-prolong inactivation of Na+ channels
- inhibit Ca2+ to lesser extent
- half life 24-35 hours (reduced to 15 by phenytoin, carb, phenobarbital, primidone)
- reduces valproate by 25%
- Side effects: dizziness, ataxia, blurred vision, nausea, rash, SJS |
|
|
Term
|
Definition
- "broad spectrum" AED
- partial, tonic/clonic, LGS
- inhibits Na+ channels
- enhance GABA receptors via AMPA-kinate
- Side effects: ataxia, fatigue, somnolence, weight loss
- reduces plasma levels of estradiol and OCP |
|
|
Term
|
Definition
- partial seizures
- tonic/clonic
- myoclonic in children
- IV: status epilepticus
- may prevent glutamate release
- HIGHEST SAFETY MARGIN; rapid dose titration makes lev. useful for adjunctive
- Side effects: somnolence, dizziness, asthenia
- NO drug-drug interactions |
|
|
Term
| AEDs of choice for: Partial seizure |
|
Definition
1. Carbamazepine, Phenytoin
2. Lamotrigine |
|
|
Term
| AEDs of choice: Generalized Absence Seizure |
|
Definition
1. Ethosuximide, Valproic Acid
2. Clonazepam |
|
|
Term
| AEDs of choice for: Generalized Tonic/Clonic |
|
Definition
1. Carbamazepine, Phenytoin, Valproic Acid
2. Lamotrigine, Topiramate |
|
|
Term
| AEDs of choice for: Status Epilepticus |
|
Definition
1. fosphenytoin
2. levetiracetam, phenobartbital, valproic acid |
|
|
Term
|
Definition
- location: brain stem, spinal cord, limbic system
- supraspinal analgesia, spinal analgesia, sedation, respiratory depression, euphoria, depdendence |
|
|
Term
|
Definition
- located in brainstem and spinal cord
- SOME spinal and supraspinal analgesia, meiosis, sedation, dysphoria |
|
|
Term
|
Definition
- brainstem and limbic system
- dysphoria and hallucinations |
|
|
Term
|
Definition
- Isometheptene (sympathomimetic --> vasoconstriciton)
- Dichloralphenazone (sedative)
- Acetaminophen
- 2 pills then 1 every hour; no more than 6
- mild to moderate migraine |
|
|
Term
|
Definition
- moderate to severe migraine
- activates 5HT1-B receptors on vessels
- reduces neurogenic inflammation
-MAX dose = 6 mg/attack and 10mg/week
- half life 2 hours; vasoconstriction can last 24
-interacts with serotonin, adrenergic and dopamine receptors as well (dirty drug)
-contraindicated in patients with PVD; B blockers may worsen
- GI upset: activation of central dopamine receptors
- erythromycin can interfere with ergotamine metabolism |
|
|
Term
|
Definition
- antiemetic
- improves oral absorption of migraine meds
- frequently given with ergotamine |
|
|
Term
| Dihydroergotamine (DHE 45) |
|
Definition
- acute Tx moderate- severe migraine
-semisynthetic alkaloid
-given parenterally; incompletely absorbed by GI tract
- stim. 5HT1 receptors --> vasoconstriction
- reduced neurogenic inflammation (decrease release of vasodilator/proinflammatory peptide transmitters)
- "dirty"; interacts with other receptors like ergotamine
- Side effects: GI upset, transient bradycardia, weakness in legs, VASOSPASM |
|
|
Term
|
Definition
- acute Tx moderate-severe migraine
- derivative of serotonin
- metabolized by MAO-A (DO NOT give with MAOI's)
- constriction of dilated intracranial arteries
- inhibits release of proinflammaotry mediators
- relieve nausea, vomiting, photophobia, phonophobia
- DO NOT give triptans via an IV (risk of vasospasm)
- Risk of cardiovascular adverse rxns |
|
|
Term
|
Definition
- chest and throat tightness
- difficulty breathing
- panic/anxiety
- paresthesia
- feeling of heaviness |
|
|
Term
|
Definition
- second generation triptan
- 5HT1 agonist like sumatriptan
- greater bioavailability than sumatriptan
- act peripherally on components of trigeminovascular system but also centrally: inhibits pain transmission in trigeminal nucleus (lipid soluble --> cross BBB)
- Eliminated by MAO-A and CYP1A2 |
|
|
Term
|
Definition
- dopamine antagonists
- Tx acute migraine unresponsive to triptans, DHE, analgesic
- relieve headache + anti-emetic |
|
|
Term
|
Definition
- migraine prophylactic
- only when other prophylactics fail
- semisynthetic ergot alkaloid
- metabolized in liver to active metabolite: methylergometrine
- 2-8 mg daily; orally with meals
- 5HT2 antagonist and 5HT1 agonist
- side effects: fibrosis (discontinue for a month every 6 months), cardiovascular (angina), GI, CNS: LSD- like effects (drowsy, insomnia, hyperactive) |
|
|
Term
Beta blockers
(propanolol, timolol, nadolol, metropolol) |
|
Definition
- first choice for migraine prophylaxis
- most effective: lack partial agonist activity
- fatigue, dizziness, cold extremities, dreams/nightmares, insomnia, depression
- caution with asthma and DM patients |
|
|
Term
|
Definition
- tricyclic antidepressant used for migraine prophylaxis
- downregulation of central 5HT2 and adrenergic receptors
- side effects are anti-cholinergic (dry mouth, urine retention, blurred vision, arrhythmia)
- caution with: glaucoma, BPH, heart disease |
|
|
Term
| Valproic acid:valproate sodium 1:1 |
|
Definition
- AED used for migraine prophylaxis
- facilitates GABA, modulates glutamate, inhibits Na+ and Ca2+ channels
- side effects: nause/vomiting, weakness (asthenia), somnolence, weight gain, tremor, hair loss, hepatic toxicity |
|
|
Term
| Topiramate and Gabapentin |
|
Definition
- AEDs used for migraine prophylaxis
- topiramate: paresthesia, fatigue, anorexia, diarrhea, weight loss, memory problems, nausea
- gabapentin: somnolence, asthenia, dizziness |
|
|
Term
|
Definition
- Oxygen inhalation
- ergotamine, DHE
- subcutaneous sumatriptan to abort HA |
|
|
Term
|
Definition
- NSAID
- used for gout Tx: anti-inflammatory via inhibition of prostaglandin synthesis
- GI irritation
- CNS side effects (dizziness, drowsiness, confusion) |
|
|
Term
|
Definition
- NSAID used in GOUT, also as an analgesic
- anti-inflammatory via inhibition of prostaglandin synthesis
- administered IM
- useful for severe, acute attacks of gout |
|
|
Term
|
Definition
- alkaloid; unique anti-inflammatory activity
- specific for GOUT: both acute attack and prevention of recurrence
- binds tubulin, preventing its polymerization --> reduction in leukocyte migration and phagocytosis
- inhibits production and release of pro-inflammatory glycoproteins form neutrophils
- GI side effects
- overdose: burning, throat pain, diarrhea, CNS depression
- transient leukopenia with acute usage
- chronic: risk of agranulocytosis, aplastic anemia, alopecia, myopathies, neuropathies
- expensive and GI effects can be severe (try to treat with NSAIDs and corticosteroids first) |
|
|
Term
|
Definition
- Tx for GOUT
- inhibits xanthine oxidase thus reducing uric acid formation
- does NOT stop acute attack but reduces potential for future attacks
- active metabolite oxypurinol has long half life
- at first, increased frequency of gout attacks due to breakdown of crystals as blood levels of UA fall
- elevation of liver enzymes
- allergive ractions
- inhibits hepatic metabolism of many drugs; increases half life of probenecid and theophylline |
|
|
Term
|
Definition
- Gout
- xanthine oxidase inhibitor (reduces uric acid formation)
- fewer skin problems and allergic rxns than allopurinol
- elevation of liver enzymes like allopurinol
- for patients who don't respond to allopurinol
- high cost |
|
|
Term
|
Definition
- Uricosuric agent
- inhibits anion exchange transporter: inhibits both secretion and reabsorption of uric acid therefor increasing excretion
- GI upset, skin rashes, overdose: seizures/death
- increased risk of kidney stone formation
- patients must consume adequate fluids
- not for acute gout attacks |
|
|
Term
| Probenecid drug interactions |
|
Definition
- inhibits tubular secretion of variety of drugs
- inhibits biliary secretion of rifampin
- salicylclates interfere with uricosuric effect
- combo probenecid + colchicine available |
|
|
Term
|
Definition
- uricosuric effects similar to probenecid
- GI side effects more common than probenecid
- displacement from plasma protein binding sites = numerous drug interactions |
|
|
Term
Prednisone
Methylprednisolone |
|
Definition
- corticosteroids; used for acute gout attacks
- may be given via intra-articular injection or in conjunction with NSAIDs |
|
|
Term
|
Definition
| Meats, seafood, gravies, yeast, beer, alcohol, beans, peas, lentils, oatmeal, spinach, asparagus, cauliflower, mushrooms |
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